NEW ACTIVE AND PASSIVE DRUG DELIVERY.ppt

Drug Delivery System
Basic Concepts
Classification
Types

1. DRUG DELIVERY?
ῼMethod or process of administering a pharmaceutical
compound to achieve a therapeutic effect in human or
animals.
ῼDrug delivery technologies are patent protected
formulation technologies that modify drug release
profile, absorption, distribution and elimination for the
benefit of improving product efficacy and safety, as well
as patient convenience and compliance.

2. MODE OF DRUG DELIVERY
ῼThe mode of delivery can be the difference between a
drug’s success and failure, as the choice of a drug is
often influenced by the way the medicine is administered

3. DRUG RELEASE
ῼIt is the release of drug from the dosage form in the
form of solution
ῼIt involve multiple steps of diffusion and partitioning

4. Targeting
ῼTargeting is the ability to direct the drug-loaded system
to the site of interest. Two major mechanisms can be
distinguished for addressing the desired sites for
targeting
ῼACTIVE TARGETING
ῼPASSIVE TARGETING

5. ῼConjugation of suitable biocompatible polymers to
bioactive peptides or proteins can reduce toxicity,
prevent immunogenic or antigenic side reactions,
enhance blood circulation times and improve solubility.
ῼModification of synthetic polymers or polymer
therapeutics with suitable oligopeptide sequences, on
the other hand, can prevent random distribution of drugs
throughout a patient’s body and allow ACTIVE
TARGETING.

6. CONJUGATION

7. ACTIVE DRUG DELIVERY SYSTEM
•Activation modulated drug delivery system.
•In these delivery systems ,release of drug molecules
from delivery system is activated by some physical,
chemical ,or biochemical processes (facilitated by energy
supplied externally)

8. PASSIVE DRUG DELIVERY SYSTEM
•Drug release from these delivery systems is by simple
diffusion process.
•In these systems drug release is along the concentration
gradient.
•No energy is required for activation of these systems.

9. •Some systems deliver drug by both active and passive
means For example TRANSDERMAL PATCHES
•NICOTINE PATCHES deliver drug by passive diffusion
due to the presence of small molecules
•The patches containing the drug having large molecules
require some source of activation

10. CONTROLLED DRUG DELIVERY
SYSTEMS
There are four major classes of controlled drug
delivery system
ῼ Rate pre-programmed DDS
ῼActivation modulated DDS
ῼ Feedback regulated DDS
ῼ Site targeting DDS

12. ACTIVATION MODULATED DRUG
DELIVERY SYSTEM
•PHYSICAL MEANS
•CHEMICAL MEANS
•BIOCHEMICAL MEANS

13. PHYSICAL MEAN
•Osmotic pressure activated DDS
•Hydrodynamic pressure activated DDS
•Vapour pressure activated DDS
•Mechanically activated DDS
•Magnatically activated DDS
•Sonophorasis activated DDS
•Ionitophorasis activated DDS
•Hydration activated DDS

14. CHEMICAL MEANS
•Ph activated DDS
•Ion activated DDS
•Hydrolysis activated DDS

15. BIOCHEMICAL MEANS
•Enzyme activated DDS
•Biochemical activated DDS
FEED BACK REGULATED DRUG DELIVERY SYSTEM

16. PASSIVE DRUG DELIVERY SYSTEM
•Polymer membrane permeation controlled TDDS
•Polymer matrix diffusion controlled TDDS
•Drug reservoir Gradient controlled TDDS
•Micro reservoir dissolution controlled TDDS
•Transdermal patches
•Transmucosal
•Conventional dosage forms

17. Osmotic pressure activated DDS
•Osmotic pressure activated DDS depends upon osmotic
pressure to activate the release of drugs.
•In this system the drug reservoir (either a solution or
solid formulation) is contained with in a semipermeable
housing with controlled water permeability.
•The drug is activated to release in solution form at a
constant rate through a special delivery orifice.

19. Examples
•Alzet miniosmotic pump
•Duros implant pump
•Other applications
•Vasopressin
•Acutrim tablet

20. Hydrodynamic pressure activated DDS
•In this system hydrodynamic pressure is possible source
of energy which activate the delivery of therapeutic
agent.
•In this system a collapsible impermeable container
containing the liquid drug formation inside a rigid shape
retaining housing

21. Vapour pressure activated DDS
•In this system vapour pressure is potential source of
energy to activate delivery of therapeutic agent
•In this system drug reservoir is contained inside infusion
compartment

22. EXAMPLE
•Development of an implantable infusion pump for
constant infusion of heparin in anti coagulation
treatment
•Insulin in antidiabetic medication
•Morphine for patient suffering from intense pain of
terminal cancer

23. Mechanically activated DDS
•In this system drug reservoir is a solution formulation
retained in container equipped with mechanically
activated pumping system
•A measured dose of the drug is delivered into a body
cavity through mechanical activation of drug delivery
pumping system
•The volume of the solution delivered is controllable as
small as 10 to 100 microliter

24. EXAMPLE
•Metered dose nebulizer
Use for intranasal adminstration of buserelin(a synthetic
analog of luteinizing hormone releasing hormone LHRH)
•Insulin delivery

25. Magnetically activated DDS
•In this type the drug reservoir is depression of peptide or
protein powders in a polymer matrix
•The drug delivery is through electromagnetically
triggered vibration mechanism in the polymeric device

26. EXAMPLE
•It is use to deliver protein drugs such as BOVINE SERUM
ALBUMIN

27. Sonophorasis activated DDS
•This system utilizes ultrasonic energy to activate delivery
of drugs from polymeric drug delivery device

28. Ionitophorasis activated DDS
•In this system electrical current is use to activate and
modulate diffusion of charged drug molecules across the
biological membrane like skin
•It is similar to the passive diffusion but at much
facilitated rate

29. EXAMPLE
•Transdermal delivery of insulin

30. Hydration activated DDS
•This system depends on hydration induced swelling
process to activate release of the drug
•The release of the drug is controlled by rate of swelling
of polymer matrix

31. EXAMPLE
•Syncro Mate-B implant
used for delivery of potent progestin
•Valrelease tablet
used for delivery of valium

32. pH activated DDS
•This system targets the delivery of drug only in the
region with selected pH range.
•Here Drug containing core is coated with pH sensitive
polymer combination.
•In this way the gastric fluid labile drug is protected by
encapsulating it inside a polymer membrane that resist
degradation action of gastric ph.

33. •In stomach, coating membrane resist action of gastric
fluid(pH<3) and protects the drug from acid
degradation.DDS then travels to small intestine where
intestinal fluid(pH>7.5)activate the erosion of intestinal
fluid-soluble polymeric component from coating
membrane thus leaving a micro-porous membrane which
is constructed from intestinal fluid insoluble poymer.

35. Ion activated DDS
•ionic or charged drug can be delivered by an ion
activated drug delivery system
•Such a system is prepared by first complexing an ionic
drug with an ion exchange resin containing a suitable
counter ion
•By forming a complex between
>a cationic drug + resin having a SO3 group
>an anionic drug + resin having a N(CH3)3 group

36. •Granules of drug-resin complex are formed
•These granules are then treated with an impregnating
agent i.e polyethylene glycol to reduce swelling in an
aq.envirnoment.
•Then coated, by air suspension coating, with a water-
insoluble but water permeable polymeric membrane
•In an electrolyte medium i.e gastric fluid, ion diffuses
into the system, reacts with the drug resin complex and
trigger the release of ionic drug.

37. EXAMPLE
Development of pennkinetic which permits the
formulation of liquid suspension dosage form with
sustain drug release properties for oral adminstration

38. Hydrolysis activated DDS
This system depends upon hydrolysis process to activate
the release of drug molecules.
Drug reservoir is either
encapsulated in microcapsule
homogenously dispersed in micro spheres or nano-
particles or injections
Fabricated as an implant device

39. •These systems are prepared from biodegradable or
bioerodable polymers
•Release of drug from polymer matrix is activated by
hydrolysis-induced degradation of polymer chains and
controlled by rate of polymer degradation.

40. EXAMPLE
•Development of LHRH releasing biodegradable sub
dermal implant which is design to deliver
goserelin(synthetic LHRH analog) for once a month
treatment of prostate carcinoma

41. Enzyme activated DDS
•This type of activation control drug delivery system
depend upon enzymatic process to activate the release
of drug
•Drug reservoir is either physically entrapped in micro
spheres OR chemically bound to polymer chain from
biopolymers such as albumin or polypeptide.
•Drug release is activated by enzymatic hydrolysis of
biopolymers by specific enzymes in target tissue.

42. EXAMPLE
Development of albumin
micro spheres that release
5-florouracil in a controlled
manner by protease
activated biodegradation

43. FEED BACK REGULATED DDS
•In this system the release of drug delivery system is
activated by triggering agent such as biochemical
substances.
•In the body it is also regulated by its concentration via a
some feedback mechanism
•The rate of drug release is then controlled by the
concentration of triggering agent detected by a sensor in
the feedback regulated mechanism

44. TYPES OF FEEDBACK REGULATED
DDS
•BIOEROSION REGULATED DDS
•BIORESPONSIVE DDS
•SELF REGULATING DDS

46. PASSIVE TRANSPORT
Passive transport means moving
biochemicalsand atomic or molecular
substances across the cell membrane.
Unlike active transport, this process does
not involve chemicalenergy
The four main kinds filtrationand osmosis
of passive transport are diffusion,
facilitated diffusion,.

47. PASSIVE DRUG DELIVERY SYSTEM
•Polymer membrane permeation controlled TDDS
•Polymer matrix diffusion controlled TDDS
•Drug reservoir Gradient controlled TDDS
•Micro reservoir dissolution controlled TDDS
•Transdermal patches
•Transmucosal
•Conventional dosage forms

48. PASSIVE DRUG DELIVERY SYSTEM
•Polymer membrane permeation controlled TDDS
•Polymer matrix diffusion controlled TDDS
•Drug reservoir Gradient controlled TDDS
•Micro reservoir dissolution controlled TDDS
•Transdermal patches
•Transmucosal
•Conventional dosage forms

49. TECHNOLOGGIES FOR DEVELOPING
TRANSDERMALDRTEMUG DELIVERY
SYSTEMS
There are four types
1.Polymer membrane permeation controlled
TDD system.
2.Polymer matrix diffusion controlled TDD
system.
3.Drug reservior gradient controlled TDD
system.
4.Microreservior dissolution controlled TDD
system.

50. POLYMER MEMBRANE
PERMEATION CONTROLLED
TDD SYSTEM
•Drug sandwitched between drug
impermeable backing laminate and rate
controlling polymeric membrane.
•EXAMPLES:
•Percutaneous absorption of prostaglandin
derivatives

51. 2.Polymer matrix diffusion
controlled TDD system
•Medicated disk
Solid drug dispersed in hydrophilic or
lipophilic polymer matrix
Example:
1.Minitran system
2.Nitro dur II system

52. 4.Microreservior dissolution
controlled TDD system
•HYBRID OF Reservoir andmatrix system
•High shearing forces required

53. 3.Drug reservior gradient controlled
TDD system
Thickness of diffusional path increases with
time.
To compensate time deopendent diffusional
path as a result of drug depletion the
loading level in the multilaminate adhesive
layers designed to increase proportionally.
EXAMPLES:
Deponit system.

55. Inner ear drug delivery for
auditory application

56. Generating and loading of
liposomal system for drug delivery

57. Active targetting the particulate
drug carriers in tumors therapy

58. Mitochondrial drug delivery for
therapeutical applications

59. For delivery of malarial vaccines

60. For delivery of antharax vaccines

61. For vitamin B12 administration to
check biological responses

62. For delivery of peptide drugs to
CNS

63. •Some drug patches
like nicotine,estrogen
and nitroglycerine are
delivered only by
passive means
because of small drug
molecules

64. •Passive transdermal
DDS provide
advantages over
other drug delivery
methods by delivering
drug directly to the
affected area

65. •For nasal drug
delivery
•Enhanced
permeability and
retention effects

66. •Active drug delivery is used for treatment
of Diabetes(insulin pump)
•Active drug delivery is also used for
treatment of cancerous tumors
•Active drug is used for antibody
medication